Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 7 of 7 for “"covalent inhibitor"”.
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Design and Synthesis of Covalent Inhibitors as Novel Anti-Infective Compounds
… describes approaches to develop selective, covalent inhibitors of enzymes in infectious diseases.<br/><br/> Covalent inhibitors are drugs which are capable of forming a covalent bond to their target. This can give them many advantages over traditional, non-covalent drugs from a …
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THE BIOTRANSFORMATION OF BILE ACIDS BY A COMMON MEMBER OF THE BISON GUT MICROBIOME
… member of this enzyme family with a pan-family inhibitor. BSHAc showed optimum activity at ~57 °C and between pH 5 and 6. Steady-state kinetic characterization of BSHAc using glycine and taurine conjugates of cholic (CA) and deoxycholic acid (DCA) revealed it was a so-called broad spectrum BSH …
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Investigations of Novel Mechanisms of Action for Anti-Bacterial and Anti-Cancer Agent Development
… on the development of a substrate-competitive covalent inhibitor for protein kinase B (AKT). AKT is a valid target for cancer research with two compounds currently in late stage clinical trials. Developing substrate- competitive inhibitors for kinases is a novel approach in targeting them, with …
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Protein degradation from the endoplasmic reticulum in yeast
… of unfolded proteins, we used a novel covalent inhibitor of de-ubiquitinating enzymes, ubiquitin-vinyl-sulfone. This inhibitor modifies 6 polypeptides in a yeast lysate, all 6 of which are known or putative de-ubiquitinating enzymes. The expression of these 6 de-ubiquitinating enzymes …
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Preclinical Studies of A Novel Idh1 Inhibitor In Acute Myeloid Leukemia (Aml)
<p><strong><strong>LY3410738, </strong>a novel covalent Isocitrate Dehydrogenase 1 (IDH1) inhibitor in Acute Myeloid Leukemia, it</strong> <strong>is more effective than Ivosidenib (AG120) and has a potent anti-leukemic effect against IDH1 mutant acute myeloid leukemia in combination with …
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QUANTITATIVE PROTEOMIC APPROACHES TO STUDY DRUG MECHANISM OF ACTION
In recent years an increased number of covalent protein kinase inhibitors has been approved for cancer therapy and many more are undertaking clinical trials. Covalent binding is usually obtained by introducing in these drugs an electrophilic warhead able to bind specific nucleophilic sites in the …
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Discovery and optimization of inhibitors and probes that target New Delhi metallo-[beta]-lactamase
… the β-lactam substrate. Codrugs in the form of covalent inhibitors that target this nucleophilic serine are prescribed along β lactam antibiotics to counteract this form of resistance. However, an emerging class of β lactamases, known as metallo-β-lactamases (MBLs), poses a threat to this …